Assay Detail
Binding
CHEMBL4253390
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Inhibition of CDK1/Cyclin-A2 (unknown origin) using histone-H1 as substrate after 90 mins by ADP-Glo assay
34
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 7 — Homologous single protein target |
| Curated By | Intermediate |
Publication
A highly potent CDK4/6 inhibitor was rationally designed to overcome blood brain barrier in gliobastoma therapy.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 34 | 6.60 | 7.57 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4284941 | — | — | 1 | 7.57 |
| CHEMBL4279791 | — | — | 1 | 7.30 |
| CHEMBL4279275 | — | — | 1 | 7.27 |
| CHEMBL4278904 | — | — | 1 | 7.19 |
| CHEMBL4288327 | — | — | 1 | 7.09 |
| CHEMBL4280423 | — | — | 1 | 7.08 |
| CHEMBL4292139 | — | — | 1 | 7.02 |
| CHEMBL4293340 | — | — | 1 | 7.00 |
| CHEMBL4291541 | — | — | 1 | 6.96 |
| CHEMBL4284737 | — | — | 1 | 6.95 |
| CHEMBL4289967 | — | — | 1 | 6.90 |
| CHEMBL4284301 | — | — | 1 | 6.88 |
| CHEMBL4286823 | — | — | 1 | 6.87 |
| CHEMBL4288134 | — | — | 1 | 6.85 |
| CHEMBL4281514 | — | — | 1 | 6.82 |
| CHEMBL4277525 | — | — | 1 | 6.82 |
| CHEMBL4292616 | — | — | 1 | 6.78 |
| CHEMBL4279832 | — | — | 1 | 6.75 |
| CHEMBL4280895 | — | — | 1 | 6.67 |
| CHEMBL4276993 | — | — | 1 | 6.63 |
| CHEMBL4284768 | — | — | 1 | 6.57 |
| CHEMBL4285830 | — | — | 1 | 6.49 |
| CHEMBL4287743 | — | — | 1 | 6.48 |
| CHEMBL4294940 | — | — | 1 | 6.38 |
| CHEMBL4290839 | — | — | 1 | 6.36 |
| CHEMBL4287693 | — | — | 1 | 6.04 |
| CHEMBL4282981 | — | — | 1 | 6.01 |
| CHEMBL4283885 | — | — | 1 | 5.98 |
| CHEMBL4288165 | — | — | 1 | 5.97 |
| CHEMBL4286100 | — | — | 1 | 5.94 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4284941 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL4279791 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL4279275 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL4278904 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL4288327 | — | IC50 | = | 82.0 | nM | 7.09 |
| CHEMBL4280423 | — | IC50 | = | 84.0 | nM | 7.08 |
| CHEMBL4292139 | — | IC50 | = | 96.0 | nM | 7.02 |
| CHEMBL4293340 | — | IC50 | = | 101.0 | nM | 7.00 |
| CHEMBL4291541 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL4284737 | — | IC50 | = | 112.0 | nM | 6.95 |
| CHEMBL4289967 | — | IC50 | = | 125.0 | nM | 6.90 |
| CHEMBL4284301 | — | IC50 | = | 131.0 | nM | 6.88 |
| CHEMBL4286823 | — | IC50 | = | 135.0 | nM | 6.87 |
| CHEMBL4288134 | — | IC50 | = | 142.0 | nM | 6.85 |
| CHEMBL4277525 | — | IC50 | = | 152.0 | nM | 6.82 |
| CHEMBL4281514 | — | IC50 | = | 153.0 | nM | 6.82 |
| CHEMBL4292616 | — | IC50 | = | 166.0 | nM | 6.78 |
| CHEMBL4279832 | — | IC50 | = | 176.0 | nM | 6.75 |
| CHEMBL4280895 | — | IC50 | = | 216.0 | nM | 6.67 |
| CHEMBL4276993 | — | IC50 | = | 234.0 | nM | 6.63 |
| CHEMBL4284768 | — | IC50 | = | 268.0 | nM | 6.57 |
| CHEMBL4285830 | — | IC50 | = | 327.0 | nM | 6.49 |
| CHEMBL4287743 | — | IC50 | = | 328.0 | nM | 6.48 |
| CHEMBL4294940 | — | IC50 | = | 417.0 | nM | 6.38 |
| CHEMBL4290839 | — | IC50 | = | 436.0 | nM | 6.36 |
| CHEMBL4287693 | — | IC50 | = | 915.0 | nM | 6.04 |
| CHEMBL4282981 | — | IC50 | = | 966.0 | nM | 6.01 |
| CHEMBL4283885 | — | IC50 | = | 1056.0 | nM | 5.98 |
| CHEMBL4288165 | — | IC50 | = | 1071.0 | nM | 5.97 |
| CHEMBL4286100 | — | IC50 | = | 1160.0 | nM | 5.94 |
| CHEMBL4289226 | — | IC50 | = | 1444.0 | nM | 5.84 |
| CHEMBL4291740 | — | IC50 | = | 2224.0 | nM | 5.65 |
| CHEMBL4289350 | — | IC50 | = | 2239.0 | nM | 5.65 |
| CHEMBL4277900 | CROZBACICLIB | IC50 | = | 2707.0 | nM | 5.57 |